ArticleJournal of the American Chemical Society2009
Broad-spectrum antimicrobial peptides by rational combinatorial design and high-throughput screening: the importance of interfacial activity.
Article in Journal of the American Chemical Society, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 130 papers.
What it found
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Who cites it
130 citing papers in PubMed.
- Precise Construction of an Antimicrobial Peptide Targeting Bacterial Cell Membranes Derived From Natural Peptides.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- One-Step Design of Potent and Nonhemolytic Antimicrobial Peptides by Using a Database-Guided, Nonmachine Learning Approach.ACS infectious diseases · 2026Article
- Antimicrobial peptides in the era of resistance: integrating AI-driven design, host-microbe interactions, and nanotechnological delivery.Frontiers in microbiology · 2026Review
- Structural pores not required: Antimicrobial peptides induce ion permeabilization of lipid membranes through transient water channels.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Cathelicidin AS-12W Derived from the Alligator sinensis and Its Antimicrobial Activity Against Drug-Resistant Gram-Negative Bacteria In Vitro and In Vivo.Probiotics and antimicrobial proteins · 2025Article
- Inhibitory effects of berberine againstMicrobiology spectrum · 2025Article
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- The effects of cyclic peptide [R4W4] in combination with first-line therapy on the survival ofFrontiers in cellular and infection microbiology · 2025Article
- Effective Immobilization of Novel Antimicrobial Peptides via Conjugation onto Activated Silicon Catheter Surfaces.Pharmaceutics · 2024Article
- Screening antimicrobial peptides and probiotics using multiple deep learning and directed evolution strategies.Acta pharmaceutica Sinica. B · 2024Article
- The evolution of antimicrobial peptide resistance in Pseudomonas aeruginosa is severely constrained by random peptide mixtures.PLoS biology · 2024Article
- Identification, Synthesis, and In Vitro Activities of Antimicrobial Peptide from African Catfish against the Extended-Spectrum Beta-Lactamase (ESBL)-ProducingPharmaceutics · 2024Article
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- The use of combination therapy for the improvement of colistin activity against bacterial biofilm.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2024Review
- Design, synthesis and structure-activity relationship (SAR) studies of an unusual class of non-cationic fatty amine-tripeptide conjugates as novel synthetic antimicrobial agents.Frontiers in pharmacology · 2024Article
- Antibacterial Activity of Rainbow Trout Plasma: In Vitro Assays and Proteomic Analysis.Animals : an open access journal from MDPI · 2023Article
- A small-molecule membrane fluidizer re-sensitizes methicillin-resistantAntimicrobial agents and chemotherapy · 2023Article
- Combinatorial Screening of Cationic Lipidoids Reveals How Molecular Conformation Affects Membrane-Targeting Antimicrobial Activity.ACS applied materials & interfaces · 2023Article
- Structure-Activity Relationships of Cationic Lipidoids againstAntibiotics (Basel, Switzerland) · 2023Article
70 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
We recently described 10 peptides selected from a 16,384-member combinatorial library based on their ability to permeabilize synthetic lipid vesicles in vitro. These peptides did not share a common sequence motif, length, or net charge; nonetheless, they shared a mechanism of action that is similar to the natural membrane permeabilizing antimicrobial peptides (AMP). To characterize the selected peptides and to compare the activity of AMPs in vivo and in vitro, we report on the biological activity of the same selected peptides in bacteria, fungi, and mammalian cells. Each of the peptides has sterilizing activity against all classes of microbes tested, at 2-8 microM peptide, with only slight hemolytic or cytotoxicity against mammalian cells. Similar to many natural AMPs, bacteria are killed within a few minutes of peptide addition, and the lethal step in vivo is membrane permeabilization. Single D-amino acid substitutions eliminated or diminished the secondary structure of the peptides, and yet, they retained activity against some microbes. Thus, secondary structure and biological activity are not coupled, consistent with the hypothesis that AMPs do not form pores of well-defined structure in membranes but rather destabilize membranes by partitioning into membrane interfaces and disturbing the organization of the lipids, a property that we have called "interfacial activity". The observation that broad-spectrum activity, but not all antimicrobial activity, is lost by small changes to the peptides suggests that the in vitro screen is specifically selecting for the rare peptides that have broad-spectrum activity. We put forth the hypothesis that methods focusing on screening peptide libraries in vitro for members with the appropriate interfacial activity can enable the design, selection, and discovery of novel, potent, and broad-spectrum membrane-active antibiotics.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.